Antiproliferative activities of alkaloid-like compounds

Xu, X; Rawling, T; Roseblade, A; Bishop, R; Ung, AT

Antiproliferative activities of alkaloid-like compounds

Xu, X

Rawling, T

Roseblade, A

Bishop, R Ung, AT

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Publication Type:: Journal Article
Citation:: MedChemComm, 2017, 8 (11), pp. 2105 - 2114
Issue Date:: 2017-01-01

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Field	Value	Language
dc.contributor.author	Xu, X https://orcid.org/0000-0003-3433-1812	en_US
dc.contributor.author	Rawling, T https://orcid.org/0000-0002-6624-6586	en_US
dc.contributor.author	Roseblade, A https://orcid.org/0000-0002-2368-9336	en_US
dc.contributor.author	Bishop, R	en_US
dc.contributor.author	Ung, AT https://orcid.org/0000-0002-5665-0702	en_US
dc.date.available	2017-10-20	en_US
dc.date.issued	2017-01-01	en_US
dc.identifier.citation	MedChemComm, 2017, 8 (11), pp. 2105 - 2114	en_US
dc.identifier.issn	2040-2503	en_US
dc.identifier.uri	http://hdl.handle.net/10453/119718
dc.description.abstract	© 2017 The Royal Society of Chemistry. Tricyclic alkaloid-like compounds were synthesised in a few steps, via the bridging Ritter reaction. The compounds were evaluated for their antiproliferative activity against the MCF-7 and the aggressive MDA-MB-231 breast cancer cells. The anti-cancer activities of 2c were found to be selective towards the aggressive and more challenging to treat triple negative (MDA-MB-231) cell line while exhibiting no antiproliferative activities towards the MCF-7 cells at the highest concentration tested (50 μM). The IC50 of compound 2c was determined to be 7.9 μM for the MDA-MB-231 cell line. Furthermore, 2c arrested cell cycle at the G2/M phase and induced apoptosis in a dose-dependent manner. Besides in-house anti-cancer screening, compound 3 was selected for anti-cancer screening by the National Cancer Institute and was found to have broad anti-cancer activity with selectivity against particular leukaemia, colon, melanoma, and breast cancer cell lines. Cytotoxicities of compounds 2c and 3 were also tested against noncancerous mammalian cells (VERO cell line), and found to be selective towards cancerous cells. The facile synthetic route, unique chemical structures and the biological data make these alkaloid-like compounds worthwhile lead compounds for further anti-cancer drug development.	en_US
dc.relation.ispartof	MedChemComm	en_US
dc.relation.isbasedon	10.1039/c7md00435d	en_US
dc.title	Antiproliferative activities of alkaloid-like compounds	en_US
dc.type	Journal Article
utslib.citation.volume	11	en_US
utslib.citation.volume	8	en_US
utslib.for	0304 Medicinal and Biomolecular Chemistry	en_US
utslib.for	0305 Organic Chemistry	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Science
pubs.organisational-group	/University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences
pubs.organisational-group	/University of Technology Sydney/Strength - CCET - Centre for Clean Energy Technology
utslib.copyright.status	closed_access
pubs.issue	11	en_US
pubs.publication-status	Published	en_US
pubs.volume	8	en_US

Abstract:

© 2017 The Royal Society of Chemistry. Tricyclic alkaloid-like compounds were synthesised in a few steps, via the bridging Ritter reaction. The compounds were evaluated for their antiproliferative activity against the MCF-7 and the aggressive MDA-MB-231 breast cancer cells. The anti-cancer activities of 2c were found to be selective towards the aggressive and more challenging to treat triple negative (MDA-MB-231) cell line while exhibiting no antiproliferative activities towards the MCF-7 cells at the highest concentration tested (50 μM). The IC50 of compound 2c was determined to be 7.9 μM for the MDA-MB-231 cell line. Furthermore, 2c arrested cell cycle at the G2/M phase and induced apoptosis in a dose-dependent manner. Besides in-house anti-cancer screening, compound 3 was selected for anti-cancer screening by the National Cancer Institute and was found to have broad anti-cancer activity with selectivity against particular leukaemia, colon, melanoma, and breast cancer cell lines. Cytotoxicities of compounds 2c and 3 were also tested against noncancerous mammalian cells (VERO cell line), and found to be selective towards cancerous cells. The facile synthetic route, unique chemical structures and the biological data make these alkaloid-like compounds worthwhile lead compounds for further anti-cancer drug development.

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http://hdl.handle.net/10453/119718